菊酰胺类化合物的合成及生物活性研究SynthesisandBiological.PDF

2010 年第 30 卷 有 机 化 学 Vol. 30, 2010 第 5 期, 719～725 Chinese Journal of Organic Chemistry No. 5, 719～725 ·研究论文· N-(取代噻唑-2-基)-菊酰胺类化合物的合成及生物活性研究 赵金浩 周 勇 徐旭辉 朱 烈 朱国念 程敬丽* (浙江大学农业与生物技术学院农药与环境毒理研究所 杭州 310029) 摘要 为了寻求新颖的氨基噻唑类先导化合物, 以含各种取代基的 2-氨基噻唑在其氨基位置与拟除虫菊酯类农药的活 性基团——菊酸采用亚结构对接的方法合成了 35 个 N-(取代噻唑-2-基)-菊酰胺类化合物, 经 1H NMR, ESI-MS 和元素 分析对化合物的结构进行了表征. 初步生物活性测定表明, 化合物 3d, 6a, 6d, 4a, 4b, 4c 和 4e 在 600 mg/L 下对小菜蛾具 有 100%的杀虫活性, 化合物 3d 和 7c 在 50 mg/L 下对多种常见病原菌具有显著的杀菌活性, 全部化合物没有明显的除 草活性. 关键词 N-取代噻唑菊酰胺; 杀虫活性; 杀菌活性 Synthesis and Biological Activities of N-(Substituted- thiazole-2-yl)-chrysanthemumamide Zhao, Jinhao Zhou, Yong Xu, Xuhui Zhu, Lie Zhu, Guonian Cheng, Jingli * (College of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310029) Abstract In order to find new thiazole lead compounds, thirty five N- (substituted-thiazole-2-yl)-chry- santhemumamides were synthesized from five types of chrysanthemic acids with seven substituted 2- 1 amino-thiazols. The structures of all new compounds were confirmed by H NMR, MS techniques and elemental analysis. At the concentration of 600 mg/L, compounds 3d, 6a, 6d, 4a, 4b, 4c and 4e showed insecticidal activity (100%) against Plutella xylostella Linnaeus. At the concentration of 50 mg/L, compounds 3d and 7c possessed good fungicidal activity toward the tested pathogens. All compounds have shown no herbicidal activity. Keywords N -(substituted